TBL 3 - Pain Management and Analgesics Flashcards by Katie Boyles

What drugs are considered counterirritants?

Capsaicin, Menthol, Methyl Salicylate, and Camphor

How well did you know this?

Not at all

Perfectly

What is the mechanism of counterirritants?

Desensitize thermal receptors (transient receptor potential vanilloid (TRPV)

How well did you know this?

Not at all

Perfectly

What drugs are considered prostanoids?

Thromboxane, Prostaglandins, and Prostacyclin

How well did you know this?

Not at all

Perfectly

What drugs use the COX-1 pathway?

Thromboxane and Prostaglandins

How well did you know this?

Not at all

Perfectly

What drug uses the COX-2 pathway?

Prostacyclin

How well did you know this?

Not at all

Perfectly

What drugs are considered corticosteroids?

Hydrocortisone, Prednisone, and Dexamethasone

How well did you know this?

Not at all

Perfectly

What is the MOA of corticosteroids?

Inhibit phospholipase 2.

How well did you know this?

Not at all

Perfectly

What is the MOA of acetaminophen (Tylenol)?

Unknown

How well did you know this?

Not at all

Perfectly

What are the properties of acetaminophen (Tylenol)?

Analgesic
Antipyretic
Lacks anti-inflammatory properties

How well did you know this?

Not at all

Perfectly

What is the role in therapy for acetaminophen (Tylenol)?

Opioid sparing

How well did you know this?

Not at all

Perfectly

What is the adverse effect of acetaminophen (Tylenol)?

Hepatoxicity

How well did you know this?

Not at all

Perfectly

What is the treatment for APAP/acetaminophen toxicity?

N-acetylcysteine (NAC)

How well did you know this?

Not at all

Perfectly

What is the MOA of N-acetylcysteine?

Restores glutathione

How well did you know this?

Not at all

Perfectly

What is the MOA of NSAIDs?

COX inhibitors
Inhibit prostanoid synthesis

How well did you know this?

Not at all

Perfectly

What are some adverse effects of NSAIDs?

GL ulcers and bleeds
CV disease
Nephrotoxicity
Bleeding

How well did you know this?

Not at all

Perfectly

Are NSAIDs anti-inflammatory?

Yes

How well did you know this?

Not at all

Perfectly

What is an example of a COX-2 selective NSAID?

Celecoxib

How well did you know this?

Not at all

Perfectly

What are some examples of Non-Selective NSAIDs?

Aspirin, Indomethacin, Meloxicam, Ibuprofen, Naproxen, Ketorolac, and Diclofenac

How well did you know this?

Not at all

Perfectly

What are the three drugs that induce the “Triple Whammy?”

NSAIDs + Diuretics + ACE-is

How well did you know this?

Not at all

Perfectly

Does aspirin reversibly or irreversibly bind COX enzymes?

Irreversibly

How well did you know this?

Not at all

Perfectly

What are some toxic effects of aspirin?

Uncouples oxidative phosphorylation leading to metabolic acidosis.

Respiratory alkalosis -> respriratory acidosis.

How well did you know this?

Not at all

Perfectly

What are some effects of aspirin toxicity?

Acidosis, tinnitus, bleeding, and altered mental status.

How well did you know this?

Not at all

Perfectly

What is the treatment for aspirin toxicity?

Sodium bicarbonate

How well did you know this?

Not at all

Perfectly

What are some examples of Alpha-2 Agonists?

Clonidine, Tizanidine, and Dexmedetomidine

How well did you know this?

Not at all

Perfectly

What is the MOA of Alpha-2 Agonists?

Decreases presynaptic Ca2+ influx. Increases postsynaptic K+ efflux.

What is the role in therapy for Alpha-2 Agonists?

Spasticity

What are some adverse effects of Alpha-2 Agonists?

Hypotension Bradycardia Sedation

What does Alpha-1 Agonism cause?

Constriction of vascular smooth muscle, leading to increased BP.

What does Alpha-2 Agonism cause?

Inhibits NE release from presynaptic neurons causing decreased BP and HR.

What are the MOA of TCAs?

Na+ channel blockers Inhibit NE re-uptake Inhibit serotonin (5-HT) re-uptake Alpha-1 Antagonist Anticholinergic

What are some examples of TCAs?

Amitriptyline, Nortriptyline, and Imipramine

What are the MOAs of Selective NE Re-Uptake Inhibitors (SNRIs)?

Inhibit the re-uptake of NE Inhibit the re-uptake of 5-HT

What are some examples of SNRIs?

Venlafaxine and Duloxetime

What is the MOA of Selective Serotonin Re-Uptake Inhibitors (SSRIs)?

Inhibit the re-uptake of 5-HT

What are some examples of SSRIs?

Paroxetine, Fluoxetine, Citalopram, and Sertraline

How do you treat anticholinergic presentations caused by TCAs?

Primarily symptomatic +/- benzodiazepines. Physostigmine Pyridostigmine

How do you treat Na+ channel blockade caused by TCAs?

Sodium bicarbonate.

How do you treat Alpha-1 Antagonism caused by TCAs?

Fluids +/- vasopressors.

How do you treat Serotonin Syndrome caused by TCAs?

Primarily symptomatic +/- benzodiazepines Cyproheptadine (serotonin antagonist)

What is the MOA of Sodium Channel Blockers?

Inhibits the neuron depolarization and action potential propagation leading to the inhibition of neurotransmitter release.

What are some examples of Sodium Channel Blockers?

Lidocaine and Carbamazepine

What is lidocaine used for?

Local anesthetic and opioid sparing.

What is an adverse effect of lidocaine?

Bradycardia

What is carbamazepine used for?

Trigeminal neuralgia

What are some adverse effects of carbamazepine?

Toxic epidermal necrolysis (TEN) and Steven Johnson Syndrome (SJS) Bradycardia SIADH: hyponatremia CYP inducer

What is the MOA of GABA-B agonists?

Decrease presynaptic Ca2+ influx and increase postsynaptic K+ efflux

What is an example of a GABA-B agonist?

Baclofen

What is the role in therapy of GABA-B agonists?

Spasticity

What are some adverse effects of GABA-B agonists?

CNS depression Abrupt withdrawal is associated with profound spasticity, hallucinations, fever, seizures, and hypertension.

What is the MOA of Calcium Channel Blockers?

Block presynaptic Ca2+ channels leading to a decrease in Ca2+ mediated neurotransmitter release from presynaptic neurons.

What are some examples Calcium Channel Blockers?

Gabapentin and Pregabalin

What are the roles in therapy of Calcium Channel Blockers?

Neuropathic pain from diabetes Fibromyalgia Opioid sparing regimens Seizures

What are some adverse effects of Calcium Chanel Blockers?

Dizziness, somnolence, confusion, and ataxia. Pedel edema.

What is the MOA of NMDA Antagonists?

Decreases postsynaptic depolarization

What is an example of a NMDA antagonist?

Ketamine

What role in therapy does ketamine have?

Acute pain opioid sparing regimens Chronic pain Mood disorders

What are some adverse effects of ketamine?

Confusion, delirium, dreamlike state, excitement, hallucinations, irrational behavior, and vivid imagery.

What adverse effect of NSAIDs is significant for COX-2 selective agents?

CV disease (myocardial infarction and stroke)

What major endogenous ligands to the mu receptors bind to?

Endorphin

What major endogenous ligands to kappa receptors bind to?

Dynorphin

What major endogenous ligands to delta receptors bind to?

Enkephalins

What are some examples of full mu agonists?

Codeine and morphine Oxycodone, oxymorphone, hydrodocone, and hydromorphone Methadone, fentanyl, meperidine

What are some examples of partial mu agonists?

Buprenorphine and Tramadol

What are some examples of mixed agonist/antagonists?

Buprenorphine and Nalbuphine

What are some full mu antagonists?

Naloxone, Methylnaltrexone, and Naltrexone

What are some additional properties of morphine?

Histamine release (itching/rash)

What are some additional properties of methadone?

NMDA receptor antagonism

What are some notable adverse effects of methadone?

QTc prolongation and drug interactions

What is methadone used for?

Chronic pain and opioid use disorder

What are some additional properties of fentanyl?

Serotonergic

What are some additional properties of meperidine?

Serotonergic and anticholinergic

What are some adverse effects of meperidine?

Serotonergic, anticholinergic, and neurotoxicity

What are some additional properties of tramadol?

Inhibits the re-uptake of serotonin and NE

What are some adverse effects of tramadol?

Serotonin syndrome and lowers seizure threshold.

What does the mnemonic "With seizures, I BITE my tongue" stand for?

Isoniazid, bupropion, imipenem/cilastatin, tramadol, enfluane.

What is the MOA of Naloxone?

Full mu competitive antagonist that acts centrally and peripherally.

What timeline is the duration of action of naloxone?

Short

What is the role in therapy for naloxone?

Acute opioid overdoses and toxicity.

What timeline is the duration of action of naltrexone?

Full mu competitive antagonist that acts centrally and peripherally.

What timeline is the duration of action of naltrexone?

Long

What is the role in therapy for naltrexone?

Opioid use disorder (OUD) and alcohol use disorder.

What is the MOA of methylnaltrexone?

Full mu competitive antagonist that acts peripherally.

What is the role in therapy of methylnaltraxone?

Opioid use constipation.

What is the MOA of Buprenorphine?

Partial/mixed mu-agonist that demonstrates a ceiling effect.

What is the role in therapy for buprenorphine?

Chronic pain and opioid use disorder.

What is the MOA of Nalbuphine?

Partial/mixed mu-antagonist.

What is the role in therapy of Nalbuphine?

Opioid-induced pruritis

What is Clonidine used for?

Treatment of opioid withdrawal